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Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists

CARROLL, William A ; KALVIN, Douglas M ; PEREZ MEDRANO, Arturo ; FLORJANCIC, Alan S ; YING WANG ; DONNELLY-ROBERTS, Diana L ; NAMOVIC, Marian T ; GRAYSON, George ; HONORE, Prisca ; JARVIS, Michael F

Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.4044-4048 [Periódico revisado por pares]

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Título:
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists
Autor: CARROLL, William A ; KALVIN, Douglas M ; PEREZ MEDRANO, Arturo ; FLORJANCIC, Alan S ; YING WANG ; DONNELLY-ROBERTS, Diana L ; NAMOVIC, Marian T ; GRAYSON, George ; HONORE, Prisca ; JARVIS, Michael F
Assuntos: Animals ; Biological and medical sciences ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Purinergic P2 Receptor Antagonists ; Rats ; Receptors, Purinergic P2X7 ; Structure-Activity Relationship ; Triazoles - chemistry ; Triazoles - pharmacology
É parte de: Bioorganic & medicinal chemistry letters, 2007-07, Vol.17 (14), p.4044-4048
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
Descrição: Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X(7) antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain.
Editor: Oxford: Elsevier
Idioma: Inglês

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